Benzisothiazolones as modulators of macrophage migration inhibitory factor.
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ABSTRACT:
SUBMITTER: Jorgensen WL
PROVIDER: S-EPMC3139435 | biostudies-literature | 2011 Aug
REPOSITORIES: biostudies-literature
Publications
Benzisothiazolones as modulators of macrophage migration inhibitory factor.
Jorgensen William L WL Trofimov Alexander A Du Xin X Hare Alissa A AA Leng Lin L Bucala Richard R
Bioorganic & medicinal chemistry letters 20110612 15
Substituted N-phenylbenzisothiazolones have been investigated as inhibitors of the tautomerase activity of the proinflammatory cytokine MIF (macrophage migration inhibitory factor). Numerous compounds were found to possess antagonist activity in the low micromolar range with the most potent being the 6-hydroxy analog 1w. Compound 1w and the p-cyano analog 1c were also shown to exhibit significant inhibition of the binding of MIF to its transmembrane receptor CD74. Consistently, both compounds we ...[more]
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